반응 #41938

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6-Bromo-3-methanesulfonyl-2-methyl-4-morpholin-4-yl-quinoline

compound

6-Bromo-3-methanesulfonyl-2-methyl-4-morpholin-4-yl-quinoline

trans-2-phenylcyclopropylboronic acid

potassium phosphate

→

white crystals

수율 61.3%

3-Methanesulfonyl-2-methyl-4-morpholin-4-yl-6-((1R,2R)-2-phenyl-cyclopropyl)-quinoline

수율 61.3%

반응 조건

후처리

1. 1
   온도at reflux under argon for 8 h
2. 2
   기타The crude product was purified by chromatography on silica gel in dichloromethane/ethyl acetate 5:1 with a gradient from 100:0 to 80:20

실험 절차

6-Bromo-3-methanesulfonyl-2-methyl-4-morpholin-4-yl-quinoline (compound of example 6) (300 mg, 0.78 mmol), trans-2-phenylcyclopropylboronic acid (189 mg, 1.17 mmol), potassium phosphate (496 mg, 2.33 mmol) and tetrakis(triphenylphosphine)-palladium (27 mg, 0.023 mmol) were heated at reflux under argon for 8 h. The crude product was purified by chromatography on silica gel in dichloromethane/ethyl acetate 5:1 with a gradient from 100:0 to 80:20. One obtained 202 mg (60%) of white crystals. MS: m/z=423 (M+H).

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